Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Phthalimide, Etc.) Patents (Class 514/417)
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Patent number: 5658940Abstract: Novel succinimides and maleimides are inhibitors of tumor necrosis factor .alpha. and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is methyl 3-(3',4',5',6'-tetrahydrophthalimido)-3-(3",4"-dimethoxyphenyl)propionate.Type: GrantFiled: October 6, 1995Date of Patent: August 19, 1997Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5639752Abstract: Compounds of the formula ##STR1## wherein Z is ##STR2## R.sub.1 is ##STR3## X is O, NH, or S; A, B, D, E, and F are each independently C, N, O, or S; wherein the remaining variables are defined in the specification, and the pharmaceutically acceptable salts thereof. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.Type: GrantFiled: May 20, 1994Date of Patent: June 17, 1997Assignee: Pfizer IncInventor: John Eugene Macor
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Patent number: 5633254Abstract: Synergistic mixtures which include dimethomorph and cymoxonil in a fungicidially effective aggregate amount, and the use of such mixtures in the control of plant diseases. In certain embodiments, a contact fungicide is included, along with the dimethomorph and cymoxonil in suitable ratios.Type: GrantFiled: January 11, 1996Date of Patent: May 27, 1997Assignees: Agrogene Ltd., C.T.S. Ltd.Inventor: Yigal Cohen
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Patent number: 5605923Abstract: Novel cyclohexene-ylidene derivatives of formula (I) are described herein. These compounds inhibit the production of Tumor Necrosis Factor and are useful in the treatment of disease states mediated or exacerbated by TNF production; they are also useful in the mediation or inhibition of enzymatic or catalytic activity of phosphodiesterase IV and are therefore useful in the treatment of disease states in need of mediation or inhibition thereof.Type: GrantFiled: September 29, 1994Date of Patent: February 25, 1997Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 5605914Abstract: Cyclic imides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 2-(2,6-dioxo-3-piperidinyl)-4-azaisoindoline-1,3-dione.Type: GrantFiled: June 10, 1994Date of Patent: February 25, 1997Assignee: Celgene CorporationInventor: George W. Muller
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Patent number: 5593990Abstract: The present invention comprises a group of compounds that effectively inhibit angiogenesis. More specifically, thalidomide and various related compounds such as thalidomide precursors, analogs, metabolites and hydrolysis products have been shown to inhibit angiogenesis and to treat disease states resulting from angiogenesis. Importantly, these compounds can be administered orally.Type: GrantFiled: January 13, 1995Date of Patent: January 14, 1997Assignee: The Children's Medical Center CorporationInventor: Robert D'Amato
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Patent number: 5536723Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.Type: GrantFiled: October 6, 1994Date of Patent: July 16, 1996Assignee: Brigham & Women's HospitalInventors: Joseph Loscalzo, John Cooke
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Patent number: 5534533Abstract: Novel carboxylate derivatives exhibiting phospholipase A.sub.2 inhibitory activity are disclosed, Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed: ##STR1## wherein A is hydroxy, amino, or lower alkylamino; R.sup.1 to R.sup.12 are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R.sup.1 to R.sup.12 are not hydrogen; G.sup.1 is a single bond, or a group of --(CH.sub.2).sub.x O(CH.sub.2).sub.y -- wherein x and y are independently 0-5; G.sup.2 is a single bond, oxygen, sulfur, carbonyl, etc.; G.sup.3 is alkyl, aryl, or a group of the formula: ##STR2## wherein R.sup.13 and R.sup.14 are independently hydrogen, alkyl, aryl, etc.; or R.sup.13 and R.sup.14 may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula: ##STR3## wherein Z is a carbon atom or a nitrogen atom, J, K, and L are independently hydrogen or aryl, etc.Type: GrantFiled: September 28, 1994Date of Patent: July 9, 1996Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Toshiyuki Kato, Yozo Hori
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Patent number: 5527547Abstract: Improved biocidal composition and method for controlling biofouling and microorganism population levels in recirculating water systems such as cooling towers, swimming pools or spas is disclosed and claimed. The composition comprises a hypochlorite donor and a bromide ion donor in proportions selected to maintain a mole ratio of the sum of all bromine containing species to the sum of all hypohalite species in the recirculating water of about 0.2 to about 20. The method comprises introducing into the recirculating water a mixture or combination of a hypochlorite donor and a bromide ion donor in an amount sufficient to maintain a ratio of the sum of all bromine containing species to the sum of all species in the recirculating water in the range of about 0.2 to about 20.Type: GrantFiled: April 4, 1995Date of Patent: June 18, 1996Assignee: The University of HoustonInventors: Terry V. T. Hight, Jack V. Matson, Lawrence F. Rakestraw, Zhihe Zhang, Thomas C. Kuechler
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Patent number: 5500441Abstract: A fungicidal mixture containinga) the oxime ether carboxamide of the formula I ##STR1## and b) a phthalimide derivative selected from the group of compounds II and III ##STR2## in a synergistically active amount is described.Type: GrantFiled: September 23, 1994Date of Patent: March 19, 1996Assignee: BASF AktiengesellschaftInventors: Horst Wingert, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Reinhold Saur, Klaus Schelberger, Manfred Hampel
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Patent number: 5491144Abstract: Compounds of formula I ##STR1## wherein Ar.sub.1, Ar.sub.2, A.sub.1, A.sub.2, R and X are as defined in the description, exhibit valuable pharmaceutical properties and are effective especially against diseases responsive to the inhibition of protein kinases, for example tumors. They are prepared in a manner known per se.Type: GrantFiled: December 21, 1994Date of Patent: February 13, 1996Assignee: Ciba-Geigy CorporationInventors: Uwe Trinks, Peter Traxler
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Patent number: 5470586Abstract: A method of controlling the attachment of organisms to an underwater surface is disclosed. The method comprises contacting the organisms with a compound of Formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, halogen, or hydroxyl. Antifouling coatings and cementitious compositions containing a compound of Formula I are also disclosed.Type: GrantFiled: April 11, 1994Date of Patent: November 28, 1995Assignee: Duke UniversityInventor: Donald J. Gerhart
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Patent number: 5464854Abstract: The method of treatment moderating, blocking and/or eliminating premenstrual syndrome embodies the intermittent administering of an AT1 antagonist to a female having menstrual cycles characterized predominately by during substantially the luteal phase inclusive of at least one and frequently by two or more affective and/or autonomic and/or somatic symptoms of substantially incapacitating severity(ies) proximately substantially prior to menses of a menstrual cycle. Losartan is an example of an AT1 inhibitor and is administered either orally or parenterally continuously to a female during her menstrual cycle's luteal phase.Type: GrantFiled: April 29, 1994Date of Patent: November 7, 1995Inventor: Anathony S. dePadova
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Patent number: 5455261Abstract: The present invention relates to a process for the control of fungal disease of plants by applying to the leaves of the plants:a) 2-(4-chlorobenzylidene)-5,5-diemthyl-1-(1H-1, 2,4-triazol-1-ylmethyl)-1-cyclopentanol;b) one or more fungicides suitable for protecting against the said fungal diseases and to compositions which may be used in the process.Type: GrantFiled: July 7, 1994Date of Patent: October 3, 1995Assignee: Rhone-Poulenc Secteur AgrochimieInventors: Alfred Greiner, Jean Hutt, Jacques Mugnier, Regis Pepin
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Patent number: 5447929Abstract: Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint diseases, such as, rheumatoid arthritis and ostecarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis, are described. Said compounds can be prepared either by hyclroxamidating a corresponding carboxylic acid or deprotecting a corresponding benzyloxycarbamoyl compound.Type: GrantFiled: March 17, 1994Date of Patent: September 5, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5439940Abstract: The invention relates to novel, pharmaceutically active benz[e]indene derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, further to the use of the said benz[e]indene derivatives in the treatment of certain diseases and in the preparation of pharmaceutical compositions suitable for the treatment of said diseases.The new benz[e]indene derivatives according to the invention correspond to the general formula ##STR1## wherein A represents a group of the formula alk-NR.sup.1 R.sup.2, wherein alk represents a C.sub.2-7 alkylene group optionally carrying a hydroxy substituent,R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-7 alkyl, C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, mono(C.sub.1-7)alkylamino(C.sub.1-7)alkyl, di(C.sub.1-7)alkylamino(C.sub.1-7)alkyl or C.sub.3-7 cycloalkyl; orR.sup.1 and R.sup.Type: GrantFiled: October 28, 1993Date of Patent: August 8, 1995Assignee: EGIS Gyogyszergyar Rt.Inventors: Klara Reiter nee Eszes, Zoltan Budai, Tibor Mezei, Gabor Blasko, Gyula Simig, Istvan Gyertyan, Luiza Petocz, Marton Fekete, Katalin Szemeredi, Istvan Gacsalyi, Gabor Gigler, Ludmilla Rohacas nee Zamkovaja, Maria Szecsey nee Hegedus, Eniko Szirt nee Kiszelly
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Patent number: 5409885Abstract: Stable and flowable aqueous dispersions of at least one water-insoluble material are formulated by dispersing such water-insoluble material, e.g., solid particulates of a plant protection compound, into a homogeneous, stable and flowable aqueous composition that includes (1) at least one water-soluble derivative of a plant protection active agent bearing at least one ionizable functional group and at least one hydrophilic functional group, (2) at least one nonionic surface-active agent and/or at least one aliphatic, cycloaliphatic or arylaliphatic alcohol having from 4 to 15 carbon atoms, and (3) water, this composition exhibiting optical birefringence and a yield point of at least 0.1 pascal.Type: GrantFiled: July 9, 1992Date of Patent: April 25, 1995Assignee: Rhone-Poulenc ChimieInventors: Paul-Joel Derian, Gilles Guerin, Philippe Jost
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Patent number: 5389668Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.Type: GrantFiled: January 12, 1994Date of Patent: February 14, 1995Assignee: Adir Et CompagnieInventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
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Patent number: 5376673Abstract: Isoindole compounds of the formula (I) ##STR1## wherein R.sub.1 represents hydrogen; C.sub.1 -C.sub.6 alkyl; benzyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, methylenedioxy; C.sub.2 -C.sub.8 aliphatic acyl; benzoyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyl, C.sub.2 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, trifluoromethyl, methylenedioxy;R.sub.2 -R.sub.3 are selected independently from hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; trifluoromethyl; hydroxy; nitro; amino; mono or di C.sub.1 -C.sub.4 alkylamino; cyano; C.sub.1 -C.sub.6 alkoxy; C.sub.2 -C.sub.6 alkoxycarbonyl;Y is ethylene, or a straight or branched alkylene chain containing from 3 to 6 carbon atoms, and the salts thereof of pharmaceutically acceptable acids. The compounds possess antianginal activity and are used in the preparation of medicaments for antianginal therapy.Type: GrantFiled: September 17, 1993Date of Patent: December 27, 1994Assignee: Italfarmaco S.p.A.Inventors: Alberto Sala, Silvio Levi, Francesca Benedini, Roberta Cereda, Piero Soldato
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Patent number: 5326760Abstract: Aminobutanoic acids of the following formula (I): ##STR1## where R.sup.1 -R.sup.5 are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatment and processes for preparing compounds of formula (I).Type: GrantFiled: March 15, 1993Date of Patent: July 5, 1994Assignee: Glaxo, Inc.Inventors: Andrew B. McElroy, Peter J. Brown, David H. Drewry, James M. Salovich, Frank J. Schoenen
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Patent number: 5310751Abstract: All possible stereoisomer forms and mixtures thereof of a compound of the formula ##STR1## wherein X is halogen, Y is --0-- or --S-- and R is selected from the group consisting of optionally substituted alkyl, alkenyl and alkynyl of up to 8 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, optionally substituted aryl and aralkyl of up to 14 carbon atoms and optionally substituted heterocyclic having pesticidal properties.Type: GrantFiled: July 1, 1992Date of Patent: May 10, 1994Assignee: Roussel UclafInventors: Didier Babin, Marc Benoit, Jacques Demassey, Jean-Pierre Demoute
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Patent number: 5292759Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY is O, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: October 15, 1992Date of Patent: March 8, 1994Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5288749Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.Type: GrantFiled: December 20, 1991Date of Patent: February 22, 1994Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
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Patent number: 5281617Abstract: N-succinimidyl and N-phthalimidyl esters of phenylalkanoic acid derivatives which are useful as inhibitors of HLE or HNE.Type: GrantFiled: February 5, 1993Date of Patent: January 25, 1994Assignee: Cortech, Inc.Inventors: Gary P. Kirschenheuter, John C. Cheronis
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Patent number: 5266587Abstract: The invention provides a new sub-class or organic peroxyacids comprising N-alkyl substituted peroxytrimellitimide of formula (I) in which R=hydrogen or linear or branched alkyl, which demonstrates an excellent combination of safe-handling and bleach performance rendering the sub-class particularly suitable for use as bleach and/or disinfectant in various bleach, bleach additive or washing compositions. Effective bleaching peroxyacids include those in which R=n propyl, iso-propyl, n butyl, sec-butyl, n pentyl and n heptyl. The invention also comprises processes for making the peroxyacids, compositions containing them and processes for washing and/or bleaching and/or disinfecting employing the invention peroxyacids or compositions containing them.Type: GrantFiled: August 23, 1991Date of Patent: November 30, 1993Assignee: Interox Chemicals LimitedInventors: John P. Sankey, A. Pryce James
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Patent number: 5262533Abstract: Amino O-aryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by arylation and amination at C-3"/C-4" of the cyclohexyl ring. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses.Type: GrantFiled: May 6, 1992Date of Patent: November 16, 1993Assignee: Merck & Co., Inc.Inventors: Peter J. Sinclair, Helen M. Organ, Matthew J. Wyvratt
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Patent number: 5256686Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined in the specification, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 29, 1992Date of Patent: October 26, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5238690Abstract: The present invention relates to a novel biologically pure culture of Triderma Harzianum, I-952, to biological control compositions containing same and to methods of protecting plants from the disease gray mold, caused by B. Cinera and the disease white rot caused by S. Sclerotiorum with such compositions.Type: GrantFiled: July 10, 1991Date of Patent: August 24, 1993Assignees: Peri Applications (1885) Ltd., Yissum Research Development Company of the Hebrew University of JerusalemInventors: Yigal Elad, Gilly Zimand, Ilan Chet
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Patent number: 5180420Abstract: The water dispersible granule of the present invention contains (a) a pesticidal active ingredient which is solid at room temperature, (b) an anionic surface active agent, and (c) a kaolin series clay having a volume median diameter of 2 .mu.m or more, and it exhibits a good disintegrability-in-water and a high dispersion stability.Type: GrantFiled: March 11, 1991Date of Patent: January 19, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Yasuyuki Katayama, Yasuhiko Ishimoto, Fumio Horide, Shigenori Tsuda, Fumio Nishioka
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Patent number: 5118704Abstract: Optically active or racemic compounds are provided having the formula ##STR1## where R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are defined in the specification; R.sub.1 is selected from the group consisting of ##STR2## wherein Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12, preferably 1 to 6, carbon atoms, and a is an integer of from zero to 3, for instance zero to 2; and pharmaceutically acceptable salts thereof; as dopaminergics.Type: GrantFiled: September 11, 1991Date of Patent: June 2, 1992Assignee: Whitby Research, Inc.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 5102447Abstract: The present invention relates to methods for protecting crop plants from undesirable effects of pesticides and herbicides. The roots, seeds or soil surrounding the crop plants are treated with an effective amount of phthalimide compound in conjunction with the use of an effective amount of the insecticidal compound or herbicidal compound. Compositions for so protecting crop plants also are provided.Type: GrantFiled: November 6, 1989Date of Patent: April 7, 1992Assignee: American Cyanamid CompanyInventor: Donald W. Gates
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Patent number: 5025033Abstract: A cholinesterase inhibiting agent which contains an alkylene diamine of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is a hydrogen atom or a hydrocarbon residue which may optionally be substituted, or R.sup.1 and R.sup.2 combinedly form, together with the adjacent nitrogen atom, a condensed heterocyclic group, R.sup.3 is a hydrogen atom or a hydrocarbon residue or an acyl group which may optionally be substituted and R.sup.4 is a hydrogen atom, or R.sup.3 and R.sup.4 combinedly form a group of the formula ##STR2## or --(CH.sub.2).sub.m+1 -- (m being 0, 1 or 2), A is --(CH.sub.2).sub.l -- (l being 0, 1 or 2) or --CH.dbd.CH--, X is a substituent or substituents and n is an integer of 4 to 7, or a salt thereof, which are useful as cerebral function improving agents for the prevention or treatment of senile dementia, Alzheimer's disease, Huntington's chorea, hyperkinesia, mania and so forth.Type: GrantFiled: January 25, 1989Date of Patent: June 18, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka
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Patent number: 5025005Abstract: Novel lipid derivatives of the formula ##STR1## [wherein R.sup.1 is alkyl or alkylcarbamoyl; R.sup.2 is hydrogen, hydroxy which may be substituted, amino which may be substituted or cyclic amino; R.sup.3 is a chemical binding or alkylene which may be substituted; R.sup.4 is hydrogen, alkyl or aralkyl; X and Y are independently O, S or an imino group which may be substituted, and when Y is an imino group, Y, together with the imino group represented by X or R.sup.4, may form a ring; and Z is imino or a nitrogen-containing heterocyclic ring which may be substituted] and salts thereof have inhibiting activity on platelet activating factor and are useful as a preventive or therapeutic agent for a variety of circulatory diseases and allergic disorders and also as an antineoplastic agent.Type: GrantFiled: July 23, 1990Date of Patent: June 18, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
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Patent number: 5001115Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.Type: GrantFiled: May 17, 1989Date of Patent: March 19, 1991Assignee: University of FloridaInventor: Kenneth B. Sloan
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Patent number: 4985452Abstract: A fungicifdal composition comprising a fungicidally effective amount of (i) a substituted 1-hydroxyethyl-triazole of the formula ##STR1## in which A is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--,or an addition product thereof with an acid or metal salt, and (ii) at least one member selected from the group consisting of(A) wettable sulphur,(B) a polyhalogenoalkylthio derivative,(C) a quanidine derivative,(D) an aromatic carboxylic acid derivative(E) a dithiocarbamate,(F) a benzimidazole derivative,(G) an imidazole or triazole derivative,(H) a phosphoric acid ester,(I) a tetrahydroquinoline derivative,(J) an S,N-heterocyclene compound,(K) a urea derivative,(L) a sulphonamide derivative,(M) a polyhydroxy ether derivative,(N) a triazine derivative,(O) a copper complex salt,(P) an N-formyl derivative,(Q) a morpholine derivative,(R) a quinoxaline derivative, and(S) a dicarboximide derivative.Type: GrantFiled: November 20, 1989Date of Patent: January 15, 1991Assignee: Bayer AktiengesellschaftInventors: Wilhelm Brandes, Gerd Hanssler, Paul Reinecke, Hans Scheinpflug, Graham Holmwood
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Patent number: 4975425Abstract: Foam compositions containing a herbicide or pesticide which are readily absorbed systemically by plant life are made by incorporating a gas such as air into a composition made up of an alcohol, a modified coconut acid or a blend of nonionic and anionic surfactants, water and a systemic herbicide or pesticide. These foam compositions are applied directly to plant life such as trees and are absorbed within three minutes, often within one minute.Type: GrantFiled: March 16, 1989Date of Patent: December 4, 1990Assignee: Mobay CorporationInventor: Horace G. Barnett, Jr.
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4950682Abstract: The present invention relates to synergistic arthropodicidal composition of several pyrethroidal active ingredients causing no damage to warm-blooded organisms comprising pyrethroides and piperonyl butoxide as active ingredient which comprises as pyrethroidal active ingredient 0.1-20% by weight of 1StransR-alpha-cyano-3-phenoxy-benzyl-3- (2,2-dichlorvinyl)-2,2-dimethyl/cyclopropane-cyrboxylate of the Formula I ##STR1## 0.05-10% by weight of cis-trans-tetramethrin (3,4,5,6-tetrahydrophthalimido-methyl(1RS)-cis-trans-chrysantemate) or trans-tetramethrin of the Formula II ##STR2## and a further pyrethroide, 0.Type: GrantFiled: February 6, 1989Date of Patent: August 21, 1990Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.Inventors: Laszlo Pap, Peter Sarkozi, Eva Somfai, Andras Szego, Istvan Szekely, Gyorgy Hidasi, Sandor Zoltan, Aniko Deak nee Moinar, Agnes Hegedus, Bela Bertok, Sandor Botar, Antal Gajary, Lajos Nagy
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Patent number: 4933360Abstract: Water-soluble dispersions of chlorthalidone are prepared by a process comprising:(a) forming a solution comprising a water soluble pharmaceutically acceptable polymeric carrier and a C.sub.1 -C.sub.4 alkanol,(b) dissolving chlorthalidone in the solution thus formed, and(c) removing the C.sub.1 -C.sub.4 alkanol from the solution by evaporation,the amount of said carrier being effective to suppress substantially the formation of the alkyl ether by-product from the reaction of chlorthalidone with the C.sub.1 -C.sub.4 alkanol. A preferred water soluble carrier is polyvinylpyrrolidone and a preferred C.sub.1 -C.sub.4 alkanol is methanol.Type: GrantFiled: November 8, 1985Date of Patent: June 12, 1990Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Nivedita Pandit, Stephen T. Horhota
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Patent number: 4923888Abstract: The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.1-4 acylamino group;R.sub.1 means hydrogen or a carboxyl-protective group; andR.sub.2 represents a --(CH.sub.2).sub.n --CO.sub.2 R.sub.5 group, whereinn is 1, 2, 3 or 4; andR.sub.5 stands for hydrogen or a carboxyl-protective group; orR.sub.2 means a --(CH.sub.2).sub.n --NH.sub.2 group, whereinn is 1, 2, 3 or 4of E and/or Z configurtion as well as their salts.The compounds according to the invention show a cytoprotective effect and promote the healing of the stomach ulcer. Their toxicity is low.Type: GrantFiled: September 26, 1988Date of Patent: May 8, 1990Assignee: Richter Gedeon Vegyeszeti Gyar RTInventors: Tamas Fodor, Laaszlo Dobay, Jaanos Fischer, Bela Stefkoo, Elemeer Ezer, Judit Matuz, Katalin Saghy, Laaszlo Szporny
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Patent number: 4886824Abstract: The invention relates to plant protection compositions based on a two-component system of plant fungicides, one of which is 1-[2-(2,4-dichlorophenyl)pentyl]-1H-1,2,4-triazole and the other is an N-haloalkanesulfenylphthalimide derivative.In the range from 1:3 to 1:100 the disclosed mixtures display enhanced fungicidal activities.Type: GrantFiled: July 5, 1988Date of Patent: December 12, 1989Assignee: Ciba-Geigy CorporationInventors: Wilhelm Ruess, Pierre Urech, Jurg Eberle, Theodor Staub
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Patent number: 4883806Abstract: Novel isomers and mixtures thereof of cyclopropane carboxylic acid derivatives with a 3-unsaturated side chain of the formula ##STR1## wherein A' is selected from the group consisting of (1) alkyl of 1 to 18 carbon atoms, (2) benzyl optionally substituted with at least one member of the group consisting of alkyl of 1 to 4 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, alkadienyl of 4 to 8 carbon atoms, methylenedioxy or halogen, ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl and R.sub.2 is selected from the group consisting of --CH.sub.2 --C.tbd.CH and monocyclic aryl, ##STR3## wherein a is selected from the group consisting of hydrogen and methyl and R.sub.3 is an aliphatic group of 2 to 6 carbon atoms containing at least one carbon-carbon unsaturation ##STR4## wherein a and and R.sub.3 have the above definition and R.sub.1 ' and R.sub.Type: GrantFiled: September 23, 1987Date of Patent: November 28, 1989Assignee: Roussel UclafInventors: Jacques Martel, Jean Tessier, Andre Teche
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4853407Abstract: Compounds represented by formula ##STR1## wherein Y.sup.1 and Y.sup.2 are identical or different, and respectively denote benzoylamino groups or phthalimide groups. This compound is useful for inhibition of dipeptidase.Type: GrantFiled: May 20, 1988Date of Patent: August 1, 1989Assignee: Sanraku IncorporatedInventors: Norio Shibamoto, Takeo Yoshioka, Yasuo Fukagawa, Tomoyuki Ishikura
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Patent number: 4851421Abstract: The invention relates to a biocidal fine powder with increased biocidal activity and an agricultural suspension containing the biocidal fine powder and an adjuvant selected from the group consisting of polyoxyalkylene-type nonionic surface active agents and polyoxyalkylene alkyl or alkylaryl ether phosphates or their salts.Type: GrantFiled: December 22, 1986Date of Patent: July 25, 1989Assignee: Kao CorporationInventors: Tetsuji Iwasaki, Yasushi Kamihisa
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Patent number: 4847301Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: July 27, 1988Date of Patent: July 11, 1989Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4839378Abstract: Fluorophthalimide compounds represented by the following general formula (I): ##STR1## wherein R each stands for an ethyl group or an isopropyl group, are effective for controlling diseases of agricultural plants, especially diseases caused by microorganisms belonging to the genus Rhizoctonia, represented by sheath blight of rice plants, and diseases caused by Basidomycetes.Type: GrantFiled: April 28, 1987Date of Patent: June 13, 1989Assignee: Meiji Seika Kabushiki KaishaInventors: Masao Koyama, Michiaki Iwata, Kunihiko Kurihara, Masaji Sezaki
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Patent number: 4801603Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.Type: GrantFiled: December 24, 1986Date of Patent: January 31, 1989Assignee: Eisai Co., Ltd.Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
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Patent number: 4795757Abstract: Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.Type: GrantFiled: November 20, 1986Date of Patent: January 3, 1989Assignee: Rorer Pharmaceutical CorporationInventors: John R. Regan, Jeffrey N. Barton, John T. Suh, Jerry W. Skiles
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Patent number: 4737512Abstract: Novel 4-(substituted-isoindol-2-yl)phenoxy-pentanoic and -heptanoic acids and derivatives which are useful as anti-arteriosclerotic agents are disclosed. The compounds elevate the high density lipoprotein fraction of cholesterol and also lower the low density lipoprotein fraction of cholesterol. Methods for preparing and using the compounds are included.Type: GrantFiled: October 27, 1986Date of Patent: April 12, 1988Assignee: Warner-Lambert CompanyInventor: Milton L. Hoefle